Details
Stereochemistry | RACEMIC |
Molecular Formula | C12H17NOS.ClH |
Molecular Weight | 259.795 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CCNC1(CCCCC1=O)C2=CC=CS2
InChI
InChIKey=ZUYKJZQOPXDNOK-UHFFFAOYSA-N
InChI=1S/C12H17NOS.ClH/c1-2-13-12(11-7-5-9-15-11)8-4-3-6-10(12)14;/h5,7,9,13H,2-4,6,8H2,1H3;1H
Tiletamine is a non-competitive N-methyl-d-aspartate (NMDA) receptor antagonist chemically related to ketamine and phencyclidine. A common veterinary anesthetic drug, tiletamine is currently a Schedule III controlled substance in USA. This compound exerts sedative effects in humans and animals, also having an abuse potential, toxicity and dissociative hallucinogenic properties clinically. In combination with benzodiazepine, zolazepam it is used as veterinary drug, called as telazol. Telazol is a nonnarcotic, nonbarbiturate, injectable anesthetic agent, which is indicated in cats for restraint or for anesthesia combined with muscle relaxation and in dogs for restraint and minor procedures of short duration (30 min) requiring mild to moderate analgesia. Tiletamine exerts sedative effects in humans and animals, also having an abuse potential, toxicity and dissociative hallucinogenic properties clinically.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28343145
Curator's Comment: Known to be CNS penetrant in rat. Human data not available
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL3442 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2846121 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | TELAZOL Approved UseUnknown |
PubMed
Title | Date | PubMed |
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Clinical and cardiorespiratory effects of propofol in the spotted bamboo shark (Chylloscyllium plagiosum). | 2005 Dec |
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Reversible anaesthesia of free-ranging lions (Panthera leo) in Zimbabwe. | 2005 Dec |
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Reversible immobilization of free-ranging African lions (Panthera leo) with medetomidine-tiletamine-zolazepam and atipamezole. | 2006 Apr |
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Cardiopulmonary effects of medetomidine or midazolam in combination with ketamine or tiletamine/zolazepam for the immobilisation of captive cheetahs (Acinonyx jubatus). | 2006 Dec |
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Reversible anesthesia of Southeast Asian primates with medetomidine, zolazepam, and tiletamine. | 2006 Dec |
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Pharmacokinetics of tiletamine and zolazepam (Telazol) in anesthetized pigs. | 2006 Dec |
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Chemical immobilization of adult female Weddell seals with tiletamine and zolazepam: effects of age, condition and stage of lactation. | 2006 Feb 9 |
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Effects of epidural morphine and transdermal fentanyl analgesia on physiology and behaviour after abdominal surgery in pigs. | 2006 Jan |
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Immobilization of free-ranging maned wolf (Chrysocyon brachyurus) with tiletamine and zolazepam in central Brazil. | 2006 Mar |
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Determination of constituents of Telazol--tiletamine and zolazepam by a gas chromatography/mass spectrometry-based method. | 2006 Oct 2 |
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Tiletamine-zolazepam-xylazine immobilization of fishers (Martes pennanti). | 2007 Apr |
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Immobilization of Japanese black bears (Ursus thibetanus japonicus) with tiletamine hydrochloride and zolazepam hydrochloride. | 2007 Apr |
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A comparison of anesthetic and cardiorespiratory effects of tiletamine-zolazepam-butorphanol and tiletamine-zolazepam-butorphanol- medetomidine in cats. | 2007 Fall |
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Performance measurements in endolaparoscopic infrarenal aortic graft implantation using computer-enhanced instrumentation: a laboratory model for training. | 2007 Jul-Sep |
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Effects of tiletamine-zolazepam anaesthesia on plasma antioxidative status and some haematological parameters in sheep. | 2007 Jun |
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Pseudomyxoma peritonei--two novel orthotopic mouse models portray the PMCA-I histopathologic subtype. | 2007 Jun 30 |
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Comparison of cardiovascular effects of tiletamine-zolazepam, pentobarbital, and ketamine-xylazine in male rats. | 2007 Mar |
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Tiletamine-zolazepam and xylazine is a potent cardiodepressive combination: a case report. | 2007 Nov |
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Nitric oxide and angiotensin II receptors mediate the pressor effect of angiotensin II: a study in conscious and zoletil-anesthetized rats. | 2007 Nov |
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Antagonistic effects of yohimbine in pigs anaesthetised with tiletamine/zolazepam and xylazine. | 2007 Nov 3 |
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Comparison of anesthetic and cardiorespiratory effects of tiletamine-zolazepam-butorphanol and tiletamine-zolazepam-butorphanol-medetomidine in dogs. | 2007 Summer |
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Principal component analysis for the comparison of metabolic profiles from human rectal cancer biopsies and colorectal xenografts using high-resolution magic angle spinning 1H magnetic resonance spectroscopy. | 2008 Apr 25 |
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Reversible immobilization of asiatic black bear (Ursus thibetanus) with detomidine-tiletamine-zolazepam and atipamezole. | 2008 Dec |
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Clinical and pathologic features of cynomolgus macaques (Macaca fascicularis) infected with aerosolized Yersinia pestis. | 2008 Feb |
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Effects of acepromazine and butorphanol on tiletamine-zolazepam anesthesia in llamas. | 2008 Feb |
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Effects of two different anaesthetics on serum concentrations of cortisol and luteinizing hormone in barrows and gilts. | 2008 Jan |
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Changes in minimal alveolar concentration of isoflurane following treatment with medetomidine and tiletamine/zolazepam, epidural morphine or systemic buprenorphine in pigs. | 2008 Jan |
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Echocardiographic reference ranges for sedated healthy cynomolgus monkeys (Macaca fascicularis). | 2008 Jan |
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Methods of advanced wound management for care of combined traumatic and chemical warfare injuries. | 2008 Jul 21 |
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Biomedical evaluation of free-ranging red ruffed lemurs (Varecia rubra) within the Masoala National Park, Madagascar. | 2008 Mar |
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Effects of premedication with tiletamine/zolazepam/medetomidine during general anesthesia using sevoflurane/fentanyl in swine undergoing pancreas transplantation. | 2008 Nov |
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Acute effects of an alternative electronic-control-device waveform in swine. | 2009 |
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Evaluation of anesthetic protocol for the collection of semen from captive collared peccaries (Tayassu tajacu) by electroejaculation. | 2009 Dec |
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Urinary cortisol responses to unusual events in captive chimpanzees (Pan troglodytes). | 2009 Jan |
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Insulin reduces cerebral ischemia/reperfusion injury in the hippocampus of diabetic rats: a role for glycogen synthase kinase-3beta. | 2009 Jan |
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The effects of different anesthetic agents on short electroretinography protocol in dogs. | 2009 Jun |
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In vivo properties of the proangiogenic peptide QK. | 2009 Jun 8 |
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Comparison of azaperone-detomidine-butorphanol-ketamine and azaperone-tiletamine-zolazepam for anaesthesia in piglets. | 2009 Mar |
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Biliary clearance of bromosulfophthalein in anesthetized and freely moving conscious rat. | 2009 Mar |
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A pig model of acute Staphylococcus aureus induced pyemia. | 2009 Mar 27 |
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Use of two anesthetic combinations for semen collection by electroejaculation from captive coatis (Nasua nasua). | 2009 May |
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Effects of different general anesthetics on serum hemolysis and hepatic and muscular glycogenolysis in rats. | 2009 Nov |
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Movement disorder caused by abuse of veterinary anesthesia containing tiletamine. | 2009 Oct |
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The effect of amnion-derived cellular cytokine solution on the epithelialization of partial-thickness donor site wounds in normal and streptozotocin-induced diabetic swine. | 2009 Oct 20 |
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Efficacy of strain RB51 vaccine in protecting infection and vertical transmission against Brucella abortus in Sprague-Dawley rats. | 2009 Sep |
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A serological survey of infectious disease in Yellowstone National Park's canid community. | 2009 Sep 16 |
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Dorsal arthrodesis in prepubertal New Zealand white rabbits followed to skeletal maturity: Effect on thoracic dimensions, spine growth and neural elements. | 2010 Jan |
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Use of hyaluronidase to improve chemical immobilization of free-ranging polar bears (Ursus maritimus). | 2010 Jan |
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Evaluation of three immobilization combinations in the capybara (Hydrochoerus hydrochaeris). | 2010 Jan-Feb |
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Transcriptomic analysis of the venom gland of the red-headed krait (Bungarus flaviceps) using expressed sequence tags. | 2010 Mar 29 |
Patents
Sample Use Guides
veterinary:
Dogs: In healthy dogs, an initial intramuscular dosage of 3 to 4.5 mg/lb (6.6 to 9.9 mg/kg) TELAZOL(tiletamine HCl and zolazepam HCl) is recommended for diagnostic purposes; 4.5 to 6 mg/lb (9.9 to 13.2 mg/kg) for minor procedures of short duration, such as treatment of lacerations and wounds, castrations and other procedures requiring mild to moderate analgesia. When supplemental doses of TELAZOL are required, such individual supplemental doses should be less than the initial dose, and the total dose given (initial dose plus supplemental dose or doses) should not exceed 12 mg/lb (26.4 mg/kg). The maximum safe dose is 13.6 mg/lb (29.92 mg/kg).
Cats: In healthy cats, an initial TELAZOL dosage of 4.4 to 5.4 mg/lb (9.7 to 11.9 mg/kg) is recommended for such procedures as dentistry, treatment of abscesses, foreign body removal and related types of surgery; 4.8 to 5.7 mg/lb (10.6 to 12.5 mg/kg) for minor procedures requiring mild to moderate analgesia, such as repair of lacerations, castrations and other procedures of short duration. Initial dosages of 6.5 to 7.2 mg/lb (14.3 to 15.8 mg/kg) are recommended for ovario- hysterectomy and onychectomy. When supplemental doses of TELAZOL are required, such individual supplemental doses should be given in increments that are less than the initial dose, and the total dose given (initial dose plus supplemental doses) should not exceed the maximum allowable safe dose of 32.7 mg/lb (72 mg/kg).
Route of Administration:
Intramuscular
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/3320347
Tiletamine was a potent and reversible antagonist of NMA-mediated responses without itself having major effects in low concentrations on normal membrane and synaptic pyramidal cell properties. Effects of tiletamine on synaptic transmission and on direct excitatory responses to exogenous amino acids were examined in rat hippocampal and striatal slices. In striatal slices, tiletamine inhibited the NMA-mediated, but not the spontaneous, release of [3H]acetylcholine, with an IC50 of 70 nM. In hippocampal CA1 cells, 3 microM tiletamine in the perfusate reversibly blocked the intracellularly recorded responses to ionophoretically applied NMA, but not to glutamate, quisqualate and kainate. Tiletamine, 3 to 100 microM, had no effect on the orthodromically elicited excitatory postsynaptic potential, action potential amplitude or duration, resting membrane potential, or input resistance. In Mg++-free perfusate, the excitatory postsynaptic potential was greatly augmented to give a paroxysmal depolarization shift and was reversibly blocked by 10 microM tiletamine.
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C245
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CFR |
21 CFR 522.2470
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1535216
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SUB04867MIG
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DTXSID6045539
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DBSALT001704
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C84212
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14176-50-2
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99TAQ2QWJI
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CHEMBL2110703
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99TAQ2QWJI
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26534
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m10862
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167740
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100000084938
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ACTIVE MOIETY
SUBSTANCE RECORD